TABLE 1.
Antiviral properties and cytotoxicity of JNJ-6379
| Cell line | Antiviral activitya
|
Cytotoxicityb
|
SIc | ||||||
|---|---|---|---|---|---|---|---|---|---|
| No. of expts | Median EC50 (range) (nM) | No. of expts | Median EC90 (range) (nM) | No. of expts | CC50 (nM) | No. of expts | CC90 (nM) | ||
| HepG2 | 21 | >25,000 | 21 | >25,000 | >463 | ||||
| HepG2.117 | 38 | 54 (14 to 115) | 36 | 226 (152 to >500) | 5 | >25,000 | 5 | >25,000 | >463 |
| HepG2.2.15 | 15 | 69 (28 to 121) | 12 | 241 (212 to 606) | |||||
a
The antiviral properties of JNJ-6379 were tested in a dose-response assay in stably HBV-replicating HepG2.117 and HepG2.2.15 cells. Intracellular (HepG2.117) or extracellular (HepG2.2.15) HBV DNA was extracted from cell lysates and assessed using quantitative PCR (qPCR). In each experiment, EC50 values were determined based on the mean inhibition from two wells per compound concentration. EC50, 50% effective concentration; EC90, 90% effective concentration.
b
Cytotoxicity was assessed in HepG2 cells using a resazurin readout. CC50, 50% cytotoxic concentration; CC90, 90% cytotoxic concentration.
c
SI, selectivity index (CC50/EC50) calculated with EC50 values from HepG2.117 cells.